Chemical and Pharmaceutical Research Group, Health Sciences Center, University of Vale do Itajai, Itajai.
Anticancer Drugs. 2012 Oct;23(9):883-96. doi: 10.1097/CAD.0b013e328356cad9.
Sesquiterpene lactones (SLs) constitute a large and diverse group of biologically active plant compounds that possess anti-inflammatory and antitumor activity. The subclass germacranolides is one of the major groups of SLs. It includes parthenolide, a highly cytotoxic SL that is being tested in clinical trials as an anti-cancer agent. In this review, we focus on SL antitumor activity related to cell-cycle arrest, differentiation, apoptosis induction through the intrinsic pathway, and sensitization of the extrinsic pathway. We also address the regression of tumors in response to cotreatment with conventional chemotherapeutics. We review the nuclear factor-κB-targeted anti-inflammatory activity in vitro and in vivo and relate it to the SL structural features involved in the molecular mechanisms. It is obvious that SLs are emerging as promising anticancer agents, but more investigations are required to fully understand the molecular mechanisms of known SLs in different cell death modalities and how these mechanisms contribute toward the potent antitumor and anti-inflammatory activities of SLs.
倍半萜内酯（SLs）是一大类具有生物活性的植物化合物，具有抗炎和抗肿瘤活性。倍半萜内酯的子类是大的内酯之一。它包括角鲨烯，一种高度细胞毒性的 SL，正在临床试验中作为一种抗癌药物进行测试。在这篇综述中，我们专注于与细胞周期停滞、分化、通过内在途径诱导细胞凋亡以及外在途径的敏化相关的 SL 抗肿瘤活性。我们还讨论了对肿瘤的消退的反应，以与常规化疗药物联合治疗。我们综述了体外和体内核因子-κB 靶向抗炎活性，并将其与参与分子机制的 SL 结构特征相关联。显然，SL 正在成为有前途的抗癌药物，但需要进一步的研究来充分了解不同细胞死亡方式中已知 SL 的分子机制，以及这些机制如何有助于 SL 的强大抗肿瘤和抗炎活性。
